Sermorelin
Sermorelin is a synthetic GHRH(1-29) analogue and growth hormone secretagogue that stimulates the pituitary to release endogenous growth hormone; it was once FDA-approved as Geref but is now discontinued and only available as a compounded preparation.
YADAIFTNSYRKVLGQLSARKLLQDIMSR
- Nonpolar13
- Polar9
- Acidic (−)2
- Basic (+)5
- 29 residues
H-Tyr-Ala-Asp-Ala-Ile-Phe-Thr-Asn-Ser-Tyr-Arg-Lys-Val-Leu-Gly-Gln-Leu-Ser-Ala-Arg-Lys-Leu-Leu-Gln-Asp-Ile-Met-Ser-Arg-NH2 (GHRH 1-29 amide)
Sermorelin is a synthetic peptide consisting of the first 29 amino acids of human growth hormone-releasing hormone (GHRH), the portion considered the shortest fully functional fragment of the native 44-residue hormone. It acts as a growth hormone secretagogue: by binding the GHRH receptor (GHRHR) on anterior-pituitary somatotrophs and activating the adenylate cyclase-cAMP-PKA cascade, it stimulates the synthesis and pulsatile release of the body's own growth hormone. Because secretion still occurs against the hypothalamus's somatostatin feedback, growth hormone output remains pulsatile rather than continuously elevated.
Chemically, sermorelin is a C-terminally amidated 29-residue peptide (sequence YADAIFTNSYRKVLGQLSARKLLQDIMSR-NH2) with the molecular formula C149H246N44O42S and a molecular weight of about 3358 g/mol (CAS 86168-78-7; PubChem CID 16132413; DrugBank DB00010). The acetate salt used pharmaceutically carries its own CAS number (114466-38-5). Its plasma half-life is short, on the order of 10-12 minutes after intravenous or subcutaneous administration, reflecting rapid enzymatic clearance.
Regulatory history: the branded product GEREF (sermorelin acetate) was approved by the FDA in the 1990s for the diagnostic evaluation and treatment of growth hormone deficiency, and was voluntarily discontinued by the manufacturer in 2008 for commercial reasons. In a 2013 determination the FDA stated that GEREF had not been withdrawn for reasons of safety or effectiveness. There is presently no FDA-approved finished sermorelin product; in the US it is supplied only as a compounded preparation through 503A pharmacies and 503B outsourcing facilities, dispensed by prescription, which is not equivalent to FDA marketing approval. It is not authorised as a licensed medicine in the UK.
This entry is provided as a research reference only. It does not constitute medical advice, makes no therapeutic or efficacy claims, and includes no dosing or administration guidance.
Sermorelin is a synthetic 29-amino-acid peptide corresponding to the biologically active 1-29 fragment of human growth hormone-releasing hormone (GHRH). It binds the GHRH receptor (GHRHR) on anterior pituitary somatotrophs, activating the adenylate cyclase-cAMP-PKA pathway to stimulate synthesis and pulsatile release of endogenous growth hormone. Because release remains under hypothalamic somatostatin feedback, GH output is pulsatile rather than continuously elevated.
- Human evidence
- Historical FDA-approved drug (now discontinued) with clinical literature in pediatric GH deficiency; broader claims are limited and largely from compounded/off-label use
- Regulatory status
- Not currently an FDA-approved finished drug product. The branded product GEREF (sermorelin acetate) was FDA-approved (1990s; used for the diagnostic evaluation and treatment of growth hormone deficiency) and was voluntarily discontinued by the manufacturer in 2008 for commercial reasons; the FDA later (2013) determined that GEREF was NOT withdrawn for reasons of safety or effectiveness. In the US it is now supplied only as a compounded preparation through 503A pharmacies / 503B outsourcing facilities, which is not equivalent to FDA marketing approval. Where supplied for human use in the US, compounded sermorelin is a prescription-only medicine (it is not a DEA-scheduled controlled substance). It is not authorised as a licensed medicine in the UK; sale for human use is restricted.
- Reference GHRH-receptor agonist used in research on the somatotropic (GHRH-GH-IGF-1) axis.
- Historically used as a diagnostic and therapeutic agent for evaluating pituitary growth hormone secretory capacity in growth hormone deficiency.
- Comparator in studies of growth hormone secretagogues and GHRH analogue pharmacology.
- Investigational interest in models of GH/IGF-1 signalling and ageing, framed strictly as research.
- Most common reported reaction in clinical use is local injection-site irritation (pain, redness, swelling), reported in roughly 1 in 6 patients in historical labelling.
- Less frequent reported effects include facial flushing, headache, dizziness, nausea, and rarely urticaria; serious hypersensitivity/allergic reactions are uncommon but possible.
- Current US supply is compounded rather than FDA-approved, so finished-product purity, potency, and sterility depend on the individual pharmacy and are not centrally guaranteed.
- Not a licensed medicine for human use in the UK; described here as a research reference material only, with no dosing or administration guidance.
- [1]PubChem Compound 16132413: SermorelinPubChem (NCBI)
- [2]Sermorelin - WikipediaWikipedia
- [3]Federal Register: Determination That GEREF (Sermorelin Acetate) Injection Were Not Withdrawn From Sale for Reasons of Safety or EffectivenessU.S. Federal Register / FDA
- [4]DrugBank: Sermorelin (DB00010)DrugBank